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Pharmacology 2 > 2.2 Sedatives, hypnotics, anxiolytics > Flashcards

2.2 Sedatives, hypnotics, anxiolytics Flashcards

1
Q

Sedatives fn

A

decrease activity,
moderate excitement and
calm the recipient

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2
Q

Hypnotics fn

A

produce drowsiness and facilitate the onset and maintenance of a state of sleep that resembles natural sleep and from which the recipient can be aroused easily

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3
Q

anxiety is cahracterized by

A

heightened arousal (i.e. physical symptoms such as tachycardia)

accompanied by apprehension, fear, and obsession

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4
Q

anxiety disorders include

A

phobia/panic disorder,
generalized anxiety disorder,
obsessive compulsive disorder,
post traumatic stress disorder

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5
Q

older anxiolytics and hypnotics like barbiturates fn

A

depress the CNS in a dose dependent manner, progressively producing sedation, unconsciousness, surgical anesthesia, coma, fatal respiratory cardiac depression

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6
Q

a normal sleep consists of

A

alternating NREM and REM sleep

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7
Q

NREMstages

A

4

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8
Q

Sleep cycle

A

90 min – 4NREM,1REM

– repeats several times during the night

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9
Q

NREM stage 0

A

awake –from lying down to falling asleep.

Constitutes 1-2% of sleep time

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10
Q

NREM stage 1

A

dozing–the first stage of NREM seep is drifting off,

it lasts 10 minutes and takes up about 2-5% of normal night sleep

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11
Q

NREM stage 2

A

the sleeper can be wakened easily,

stage 2 sleep occupies approximately 50% of sleep time

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12
Q

NREM stage 3

A

much more difficult to awaken,

larger slower delta brain waves are generated

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13
Q

NREM stage 4

A

during this stage of sleep the body gets its most rest,
very difficult to be awakeng and
sometimes sleep walking (somnabulism) occurs

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14
Q

slow wave sleep (SWS)

A

stages 3 and 4

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15
Q

during stages 2, 3, and 4

A

heart rate, BP, and respiration are steady and

muscles are relaxed

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16
Q

REM sleep

A

brain is extremely active,
brain waves are small and fast with bursts of activity,
REM sleep is characterized by “rapid eye movemt”, and is
the phase when dreams occur most often and intensely
(but dreams can occur at other stages too)

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17
Q

% of sleep in stage 1

A

5%

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18
Q

% of sleep in stage 2

A

40-50% — longest

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19
Q

% of sleep in stage 3

A

12%

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20
Q

% of sleep in stage 4

A

12%

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21
Q

% of sleep in REM

A

25%

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22
Q

A hypnotic, at a lower dose

A

becomes a sedative

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23
Q

classification of these drugs

A

benzodiazepines,
barbiturates,
benzo receptor agonists,
5HT1A receptor agonist

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24
Q

benzodizepines structure

A

benzene ring, diazepine ring

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25
Q

benzo TI

A

high

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26
Q

benzo and anesthsia

A

cannot induce a state of surgical anesthesia

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27
Q

benzo dependance liablity

A

low

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28
Q

benzo antidote

A

flumazenil

29
Q

benzo and induction

A

does not induce P450

30
Q

benzos act by

A

interacting with the inhibitory GABA a receptors,
has Cl channles,
bind at a distinct site on the receptor

31
Q

gaba binding to gabaA rec

A

opening of chlride channel,
leading to hyperpolarization,
increasing the firing threshold, and
decrease generation of action potential

32
Q

gaba and benzos

A

binding of gaba is enhanced by benzos resulting in a greater entry of chlroide ion due to

greater freq of opening of the channels, reducing neural excitablity

33
Q

benzo action

A

does not directly activate GABA-a rec but REQUIRES GABA to express their effects

34
Q

GABA facilitatory

A

Benzodiazepines

35
Q

benzo and Cl channels

A

inc frequency of opening of Cl channels

36
Q

BZD receptors

A

bzd binds to alpha and gamma subunits in gaba receptor

but NOT with beta subunit

37
Q

Benzo receptor tyeps

A

BZ1 BZ2

38
Q

BZ1

A

associated with alpha1 subunit.

Mediates sedation (higher dose),
anterograde amnesia,
anticonvulsant action.

Tolerance.

39
Q

BZ2

A

associated with alpha2 subunit.

Mediates antianxiety action, (low doses),
muscle relaxation.

No tolerance.

40
Q

long acting benzo (1-3d)

A

flur azepam,
di azepam,
chlordi azepoxide,
chlor azepate

41
Q

intermediate acting benzo (20-20h)

A

alpr azolam,
lor azepam,
tem azepam

42
Q

short acting benzo (3-8hrs)

A

Tri azolam,
Mid azolam,
Ox azepam

43
Q

Actions of benzos

A

selective depressant actions,

NOT general depressants like barbiturates

44
Q

Benzo on CNS

A

reduction of anxiety (anxiolytic) and aggression at low dose,
sedation and induction of sleep (sedative and hypnotic),
reduction of muslce tone and co-ordination (muslce relaxant),
anti-convulsant effect,
anterograde amnesia (an impairment of memory and recall of envents occuring after the dose is taken)

45
Q

reduction of anxiety and aggression by benzo

A

at low doses, benzos are anxiolytics,
reduce anxiety by selectivley inhibiting neuronal circuits in the limbic system of the brain
(BZ2 rec mediate antianxiety and impairment of cognitive functions)

46
Q

at the the benzo receptor

A

flumazenil (antagonist) and
zolpidem (sedatives)

can bind

47
Q

Alprazolam also has

A

antidepressant actions

48
Q

Triazolam is reported to produce

A

agression

49
Q

tolerance depvelps to

A

sedative hypnotic property, and
anticonvulsant property,

NOT to anxiolytic property

50
Q

benzo and sedation and induction of sleep

A

benzo decreases time taken to get to sleep
(dec sleep latency and hasten onset of sleep),
increase duration of stage 2 NREM,
dec duration of REM sleep,
red intermittent awakening and increase total sleep time,
most subjects wake up with a feeling of refresing sleep,
sedative action is mediated through BZ1R

51
Q

benzo receptor for sedation

A

BZ1R

52
Q

benso receptor for anxiolytic

A

BZ2R

53
Q

benzo as a muscle relaxant

A

BZDs relax the spasticity of skeletal muscle,
probably by increasing presynaptic inhibition in the spinal cord.

At high dose, BZDs depress neuromuscular transmission,

BZDs muscle relaxant effect is independent of sedative action

54
Q

benzo muscle relaxants

A

clon azepam,
flunitr azepam,
di azepam

55
Q

Anticonvulsant effects of benzos

A

ihibit the development and spread of epileptic seizures in the CNS,

can exert anticonvulsant effects without marked CNS depression, so that mentation and physiologic activity are unaffected,

tolerance develops to anticonvulsant action

56
Q

anticonvulsant benzos

A

clon azepam,
di azepam,
nitr azepam, and
flur azepam

57
Q

respiratory effects of benzos

A

respiratory suppression occurs at high dose,

however no effect on normal subjects at hypnotic dose

58
Q

caution of benzos

A

COPD and asthmatic patients are more prone to respiratory depression,

also caution should be used in pts with cardiac complications

59
Q

overdose of benzos can cause

A

death due to depression of medullary respiration center

60
Q

CVS and Benzo

A

hypnotic dose in normal subjects will have no CVS effect,

pre-anesthetic dose reduces BP and HR,

Toxic dose leads to circulatory collapse due to depression in myocardial contractility (neg inotropic effect) and vascular tone

61
Q

GIT and Benzo

A

decrease nocturnal gastric secretion

62
Q

Structure of BZDs

A

lipophilic

63
Q

bzd and pregancy

A

benzos cross placental barrier - FLOPPY BABY SYNDROME,

and secreted in the milk

64
Q

most enzymes are metabolized by

A

hepatic cyp450 enzyme system to active compunds

– some undergo enterohepatic circulation

65
Q

bzds that do not have active metabolites and involve only conjugation, preferred in elderly

A

lor azepam,
ox azepam,
tem azepam

66
Q

dealkylation and hydroxylation of bzds give rise to

A

many metabolites, some of which may be active, so biological effects may be much longer than plasma half-life

67
Q

adverse effects of benzos

A

relatively safer drug,

monitor 
incoordination, 
impairment of mental and motor fn 
(driving machinery should be avoided), 
confusion, 
anterograde amnesia;

increased reaction time,
cognitive performance appears to be affected less than motor performance

68
Q

contraindication of benzos

A

pregnancy,
substance abuse,
sleep apnea

69
Q

chronic use of benzos leadst to

A

tolerance and

dependance

Pharmacology 2 (12 decks)

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